XENICAL 120

Solid gelatine capsules No. 1, opaque, turquoise. On the body of the capsule there is an inscription “XENICAL 120”, looked just like-ROCHE, black. The contents of capsules-pellets white, or almost white.

xenical medication

Pharmacological properties

Xenical-specific inhibitor of gastro-intestinal lipase, which has long-lasting effects. Its therapeutic action is performed in the lumen of the stomach and small intestine and lies in the formation of the covalent bond with active serinovym plot of gastric and pancreatic lipase. The enzyme is inactivated when it loses its ability to break down fats food coming in the form of triglycerides, free fatty acids and-absorbable monohlycerides. Since the accumulation of triglycerides is not absorbed, occurs as a consequence of this reduction in revenues of calories in the body reduces the body weight. Thus, the therapeutic action of the preparation is done without suction system in the bloodstream.
Based on fat content in Calais, action orlistata begins in 24-48 hours after admission. After preparation the fat content in feces via 48-72 hours usually returns to the level, which had occurred prior to the start of therapy.

Volunteers with normal weight and obese systemic effects of the drug. Via 8:00 after oral administration of the drug orlistat unchanged plasma cannot be determined, which means that concentrations are below the 5 ng/ml.
In General, after taking therapeutic doses of identify unmodified orlistat plasma succeeded only in rare cases, the concentrations were extremely small 10 ng/ml or 0.02 ?mol). Signs of cumulation, which confirms that the absorption of the drug.

Distribution

The volume cannot be determined, since the drug is very poorly absorbed. In vitro orlistat for more than 99% is associated with plasma proteins (mostly with lipoproteins and albumin). In minimum quantities orlistat can penetrate the erythrocytes.
Metabolism
Judging from the data obtained in the experiment on animals, metabolism orlistata is carried out mainly in the bowel wall. In a study in patients with obesity found that approximately 42% of the minimal fraction of the drug, which is a systemic absorption are two main metabolite-M1 (cetyrehclennoe gidrolizirovannoe laktonovoe ring) and M3 (M1 with otseplennym remnant of N-formillejcina).
Molecules of M1 and M3 are open-? lactonnoe ring and very weakly inhibit the lipase (respectively, 1000 and 2500 times weaker than Orlistat). Given this low activity inhibiting and low plasma concentrations (on average 26 108 ng/ml ng/ml, respectively) after taking therapeutic doses, these metabolites are considered as pharmacologically inactive.
Inferring
Studies in patients with normal and overweight have shown that the main route of elimination is nevsosavsegosa drug excretion from faeces. Faeces, about 97% is displayed at the dose of the drug, and 83% in unmodified form orlistata.
Total renal excretion of all substances that are structurally related to orlistatom is less than 2% of the dose. Time to complete elimination of the drug from the body (feces and urine) is 3-5 days. The ratio of ways of deducing orlistata volunteers with normal and overweight proved the same. Both orlistat and metabolite M1 and M3, can be subjected to excretion in the bile.
Indications for use:
1. Long-term therapy of patients with obese or overweight patients, including those associated with obesity risk factors, combined with a moderate’s a hypocaloric diet.
2. In combination with hypoglycemic drugs (metformin, sulphonylurea and/or insulin) or moderately’s a hypocaloric diet in patients with diabetes mellitus type 2 with overweight or obesity.
Xenical is effective in terms of long-term control of body weight (weight loss and keep it going at a new level, avoid repeating the increase of body weight). Ksenikalom treatment leads to improved profile of risk factors and diseases associated with obesity, including giperholesterinemiu, type 2 diabetes, impaired glucose tolerance, giperinsulinemia, arterial hypertension, and to reduce the amount of visceral fat.
When used in combination with hypoglycemic medications such as metformin, sulphonylurea and/or insulin in patients with diabetes mellitus type 2 with overweight (BMI 28 kg/m2) or obese (BMI 30 kg/m2) Xenical, combined with moderate’s a hypocaloric diet, gives additional improvement compensation carbohydrate Exchange.

Usage and dosage:

In adults, the recommended dose is one capsule orlistata 120 mg with each main meal (at the time of delivery or has not later than one hour after eating). If you miss a meal or if the food contains no fat, the reception you can also skip the Xenical. Increase dose orlistata over recommended (120 mg 3 times daily) does not lead to the strengthening of its therapeutic effect.
Dose adjustment in elderly patients is not required. Dose adjustment in violation of the liver or kidneys are not required. The safety and efficacy of Xenical have children under the age of 18 years has not been established.
Contraindications:
Chronic malabsorption syndrome, Cholestasis, hypersensitivity to the drug or any other components contained in the capsule.

Side effects:

Adverse reactions to orlistat arose mainly from the gastrointestinal tract and were attributable to the pharmacological action of the drug, preventing the absorption of fat food. Very often observed phenomena such as oily discharge from the rectum, the allocation of a certain amount of gas discharge, peremptory craving to defecation, steatorrhea, frequent defecation, loose stools, bloating, pain or discomfort in the abdomen.
Their frequency increases with increasing the fat content in the diet. Patients should be informed of the possibility of adverse reactions on the part of the gastrointestinal tract and how to resolve them through better adherence to diet, particularly in relation to the amount of fat contained therein. Use low-fat diet reduces the likelihood of side effects from the gastrointestinal tract and thereby helps patients to control and regulate the consumption of fats.
Typically, these side effects are transitory and transient. They arose in the early stages of treatment (first 3 months), and in most patients was no more than a single episode of such reactions.
Precautions:
In clinical studies the majority of patients have concentrations of vitamins A, D, E, and k and beta-karotena in the course of two full years of therapy orlistatom, remained within the normal range. To ensure an adequate supply of all nutrients, you can assign a multivitamin. If assigned to multivitamins, their better take not less than 2:00 after taking orlistata or at bedtime.
The likelihood of adverse reactions on the part of the gastrointestinal tract may increase if Xenical take amid food rich in fats (e.g. 2000 kcal/day, of which more than 30% in the form of fats, which equals approximately 67 grams of fat). The patient must receive a well-balanced, moderately gipokalorijnuu diet containing no more than 30% of energy as fat. Recommended diet, rich in fruits and vegetables. Daily consumption of fats, carbohydrates and proteins should be distributed in three main reception.

Pregnancy and breast-feeding:

Product categories in.
In reproductive toxicity studies on animals teratogenic and embryotoxic effects of the drug were observed. In the absence of teratogenic effects in animals expect such an effect in humans should not be. However, due to the lack of clinical data Xenical should not assign pregnant women.
Orlistata excretion in breast milk has not been studied, so it should not be taken during lactation.
Drug interactions:
Not detected interaction with amitriptilinom, atorvastatin is appropriate, biguanidami, digoxinom, fibratami, fluoxetine, lozartanom, oral contraceptives, phenytoin, fenterminom, pravastatinom, varfarinom, nifedipine GITS (gastro-intestinal therapeutic system) and slow release nifedipine sibutraminom or alcohol (based on studies of interactions between the drugs). However, there is a need to monitor the indicators of MNO in concomitant therapy with warfarin or other oral antikoagulyantami.
Together with the admission Ksenikalom noted reduced intake of vitamins A, D, e, k and beta-carotene. If recommended multivitamin, they should take no less than 2:00 after taking Xenical or before bedtime.
While receiving Xenical and Cyclosporine plasma Cyclosporine concentrations has decreased, so it is recommended more frequent definition of Cyclosporine concentrations in plasma while receiving Cyclosporine Xenical.
When prescribing amiodarone during therapy Ksenikalom decreased systemic exposure (dezetilamiodarona and amiodarone 25-30%), but with a complicated amiodarone, farmakokinetika clinical significance of this phenomenon is not clear. Adding Xenical to long-term therapy amiodarone may lead to reductions in the therapeutic effect of amiodarone.
Avoid the simultaneous reception of Xenical and acarbose, due to the lack of data farmakokineticeskih research.
Overdose:
In clinical studies in patients with normal weight and obese patients receiving single doses of 800 mg or multiple dose of 400 mg 3 times a day for 15 days has not been accompanied by the emergence of significant adverse events.